Talabostat mesylate

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Cat.No. 3719 - Talabostat mesylate | C9H19BN2O3.CH3SO3H | CAS No. 150080-09-4
Description: Potent DPP IV inhibitor; activates NLRP1b inflammasome
Alternative Names: Val-boroPro, BXCL 701
Chemical Name: B-[(2R)-1-[(2S)-2-Amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]boronic acid methanesulfonate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent DPP IV inhibitor (IC50 values are <4, 4, 11, 310 and 560 nM at DPP4, DPP8, DPP9, DPP7 and FAP, respectively). Activates the inflammasome sensor protein NLRP1b and selectively triggers pyroptosis in monocytes and macrophages. Induces immune-mediated tumor regression in multiple mouse models of cancer. Orally bioavailable.

Technical Data

M. Wt 310.18
Formula C9H19BN2O3.CH3SO3H
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 150080-09-4
PubChem ID 11522448
InChI Key OXYYOEIGQRXGPI-WSZWBAFRSA-N
Smiles O=C([C@@H](N)C(C)C)N1CCC[C@H]1B(O)O.CS(O)(=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 31.02 100
DMSO 31.02 100

Preparing Stock Solutions

The following data is based on the product molecular weight 310.18. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.22 mL 16.12 mL 32.24 mL
5 mM 0.64 mL 3.22 mL 6.45 mL
10 mM 0.32 mL 1.61 mL 3.22 mL
50 mM 0.06 mL 0.32 mL 0.64 mL

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References

References are publications that support the biological activity of the product.

Okondo et al (2017) DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat.Chem.Biol. 13 46 PMID: 27820798

Okondo et al (2018) Inhibition of Dpp8/9 activates the Nlrp1b inflammasome. Cell Chem.Biol. 25 262 PMID: 29396289


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Keywords: Talabostat mesylate, Talabostat mesylate supplier, Potent, DPP, IV, inhibitors, inhibits, inflammasome, pyroptosis, Nlrp1b, BXCL701, DPP4, Val-boroPro, BXCL, 701, Dipeptidyl, Peptidase, (DPP-IV), Inflammasomes, Other, Apoptosis, 3719, Tocris Bioscience

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